Pentoxifylline solution concentrate for infusion 20 mg/ml 5 ml ampoules, 10 pcs.

Composition

Active ingredient:pentoxifylline — 20 mg;

Auxiliary substances:sodium chloride-6 mg, sodium dihydrogen phosphate dihydrate (sodium phosphoric acid monosubstituted 2-water) – 1 mg,0.1 M sodium hydroxide solution up to pH 6.0-8.0, water for injection up to 1 ml

. Pharmacological action

Pharmacotherapeutic group: vasodilator. ATX code[C04AD03]Pharmacological Propertiespharmacodynamicapentoxifylline is a derivative of xanthine. Improves microcirculation and rheological properties of blood. The mechanism of action is associated with inhibition of phosphodiesterase and an increase in the content of cyclic 3,5-adenosine monophosphate (3,5-AMP) in platelets and adenosine triphosphate (ATP) in red blood cells with simultaneous saturation of the energy potential, which in turn leads to vasodilation, a decrease in total peripheral vascular resistance, an increase in systolic and minute blood volume without significant changes in heart rate. By dilating the coronary arteries, it increases oxygen delivery to the myocardium (a slight antianginal effect), and improves blood oxygenation in the lungs. When administered intravenously, it leads to increased collateral blood circulation, an increase in the volume of blood flowing through the unit section. Reduces blood viscosity, causes platelet disaggregation, increases the elasticity of red blood cells (by affecting the pathologically altered deformability of red blood cells). Improves microcirculation in areas of impaired blood circulation. With occlusive damage to the peripheral arteries (“intermittent” claudication), it leads to an extension of the walking distance, elimination of night cramps of the calf muscles and pain at rest. Pharmacokinetics The drug is rapidly metabolized in the liver after administration. In the process of metabolism, two main metabolites are formed: 1-(5-hydroxyhexyl) – 3,7-dimethylxanthine (metabolite I) and 1-(3-carboxypropyl)-3,7-dimethylxanthine (metabolite V), which have similar activity to pentoxifylline.1.5-2 hours after the infusion, the concentration of metabolites I and V in the blood plasma is 5 and 8 times higher than the concentration of the initial substance, respectively. By the 8th hour, the concentration of pentoxifylline and its metabolites in the blood significantly decreases (up to 10% of the initial level). The elimination half-life is from 30 minutes to 1.5 hours. It is mainly excreted by the kidneys (94%) in the form of metabolites (mainly metabolite V), by the intestines (4%). up to 90% of the dose is eliminated in the first 4 hours.2% of the drug is excreted unchanged. Pentoxifylline and its metabolites do not bind to plasma proteins. It is excreted in breast milk. In severe renal impairment, the excretion of metabolites is slowed down. With impaired liver function, there is an elongation of the elimination half-life and an increase in bioavailability.

Indications

• Peripheral circulatory disorders in the background of atherosclerotic, diabetic and inflammatory processes (including in the “intermittent” claudication due to atherosclerosis, diabetic angiopathy, obliterative endarteritis);
• trophic disorders of the tissues due to disorders of the blood microcirculation and venous (varicose ulcers, gangrene, frostbite);
• angioneurotic (paresthesia, acrocyanosis, Raynaud’s disease);
• acute and chronic disorders of cerebral circulation ischemic type (i. e. cerebral arteriosclerosis);
• condition after hemorrhagic or ischemic stroke;
• violation of blood circulation in the vessels of the eye (acute and chronic insufficiency of retinal blood vessels and membranes of the eyes);
• dysfunction of the middle ear vascular origin, accompanied by hearing loss.

Use during pregnancy and lactation

Pentoxifylline is contraindicated during pregnancy, because the experience of using the drug in pregnant women is limited.

If it is necessary to prescribe Pentoxifylline during lactation, breast-feeding should be discontinued due to the fact that pentoxifylline penetrates into breast milk (according to the section “Pharmacokinetics”).

Contraindications

• Hypersensitivity to pentoxifylline or other xanthine derivatives, as well as other components of the drug;
• pronounced coronary or cerebral arteriosclerosis;
• acute myocardial infarction;
• severe heart rhythm disorders;
• uncontrolled arterial hypotension;
• bleeding;
• bleeding in the retina of the eye;
• a brain haemorrhage;
• ulcer disease of stomach and duodenum;
• the violation of indicators of blood coagulation;
• pregnancy;
• breastfeeding;
• age to 18 years (efficacy and safety not established).

Use caution in patients with labile blood pressure, a tendency to hypotension, chronic heart failure, a tendency to hemorrhage, a condition after recent surgical interventions, with severe hepatic and/or renal insufficiency (creatinine clearance less than 10 ml / min). Patients with connective tissue diseases (including systemic lupus erythematosus). Pentoxifylline should be administered with caution in combination with direct and indirect anticoagulants due to the increased effect of the latter.

Side effects

The frequency of possible side effects listed below is determined as follows: very common (≥1/10); common (≥1/100 to < 1/10); uncommon (≥1/1000 to < 1/100); rare (≥1/10000 to < 1/1000); very rare (Disorders of the blood and lymphatic system:Very rare: thrombocytopenia, thrombocytopenic purpura, aplastic anemia, pancytopenia. Rarely: bleeding (including nosebleeds, gastrointestinal bleeding, bleeding from the urinary tract, etc. ). Immune system disorders:Infrequently: hypersensitivity reactions. Very rare: severe anaphylactic or anaphylactoid reactions occurring within a few minutes after pentoxifylline administration, angioedema, bronchospasm, anaphylactic shock. Mental disorders:Infrequently: increased excitability, insomnia. Nervous system disorders:Infrequently: dizziness, tremor, headache. Very rare: paresthesia, convulsions, intracranial hemorrhage, aseptic meningitis. Visual disturbances:Infrequently: visual impairment, conjunctivitis. Very rare: retinal hemorrhage, retinal detachment. Cardiac disorders:Infrequently: cardiac arrhythmia, tachycardia. Rarely: angina pectoris, shortness of breath. Vascular disorders:Often: hyperemia of the facial skin. Rarely: low blood pressure, peripheral edema. Very rare: increased blood pressure. Disorders of the gastrointestinal tract:Often: nausea, vomiting, bloating, feeling of heaviness in the stomach, diarrhea. Liver and biliary tract disorders:Very rare: intrahepatic cholestasis, increased activity of “hepatic” transaminases. Skin and subcutaneous tissue disorders:Infrequently: pruritus, erythema, urticaria. Very rare: toxic epidermal necrolysis, Stephen-Johnson syndrome, increased sweating. General disorders and disorders at the injection site:Infrequently: increased body temperature.

Interaction

Pentoxifylline can enhance the effect of drugs that affect the blood coagulation system (indirect and direct anticoagulants, thrombolytics), antibiotics (including cephallosporins-cefamandol, cefoperazone, cefotetane), valproic acid. Increases the effectiveness of antihypertensive drugs, insulin, hypoglycemic agents for oral administration. Cimetidine increases the concentration of pentoxifylline in the blood plasma (risk of side effects). Co-administration with other xanthines can lead to excessive nervous excitement.

How to take, course of administration and dosage

Intravenously or intra-arterially. During the infusion, the patient should be in the “lying” position. The drug is administered intravenously drip slowly at a dose of 100 mg in 250-500 ml in 0.9% sodium chloride solution or in 5% dextrose (glucose) solution (duration of administration-90-180 minutes). The daily dose for intravenous administration can be increased to a maximum of 300 mg / day. Intra-arterial – first in a dose of 100 mg in 20-50 ml of 0.9% sodium chloride solution, and in subsequent days-200-300 mg in 30-50 ml of 0.9% sodium chloride solution (the rate of administration is 10 ml / min). With severe atherosclerosis of the cerebral vessels, the drug should not be injected into the carotid artery. Patients with chronic renal failure (creatinine clearance less than 10 ml / min) are prescribed 50-70% of the usual dose. Procedure for working with a polymer ampoule: “see the diagram on the drug packaging”, namely:1. Take the ampoule and shake it, holding it by the neck.2. Squeeze the ampoule by hand, while the drug should not be released, and rotate and separate the valve with rotating movements.3. Immediately connect the syringe to the ampoule through the resulting hole.4. Turn the ampoule over and slowly fill the syringe with its contents.5. Put the needle on the syringe.

Overdose

Symptoms: weakness, dizziness, marked decrease in blood pressure, tachycardia, drowsiness, loss of consciousness, tonic-clonic convulsions, increased nervous excitability, hyperthermia, areflexia, signs of gastrointestinal bleeding (vomiting like “coffee grounds”).

Treatment: symptomatic, aimed at maintaining respiratory function and blood pressure.

Special instructions

Treatment should be carried out under the control of blood pressure. In patients with chronic heart failure, circulatory compensation should be achieved.In diabetic patients taking hypoglycemic agents, the administration of high doses of Pentoxifylline may cause severe hypoglycemia (dose adjustment is required). When prescribed simultaneously with anticoagulants, it is necessary to carefully monitor the parameters of the blood coagulation system. In patients who have recently undergone surgery, systematic monitoring of hemoglobin and hematocrit concentrations is necessary. The administered dose should be reduced in patients with low and unstable blood pressure. Elderly patients may need to reduce the dose (increase bioavailability and decrease the rate of elimination). Smoking tobacco may reduce the therapeutic effectiveness of the drug. Compatibility of the Pentoxifylline solution with other infusion solutions should be checked on a case-by-case basis. During therapy, monitoring of the sodium content in blood plasma is required, especially in patients following a diet with a restriction of table salt (total sodium content in a 5 ml ampoule is 11.8 mg, in a 10 ml ampoule-23.6 mg. The effect on the ability to drive vehicles and mechanisms has not been studied.

Storage conditions

In a dark place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years.

Active ingredient

Pentoxifylline

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Purpose

For adults as directed by your doctor

Indications

Trophic ulcers, Consequences of stroke, Atherosclerosis, Diabetic retinopathy, Cerebral circulation disorders, Frostbite, Raynaud’s disease, Vascular lesions in diabetes mellitus, Vascular eye diseases

Weight

Weight: 116 g.